Radioiodinated Phenoxyacetic Acid Derivatives as Potential Brain Imaging Agents. II. : Structure Biodistribution Relationship

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概要

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• In developing new brain imaging agents for single photon emission computed tomography (SPECT), we synthesized eleven radioiodinated phenoxyacetic acid derivatives and investigated the relationship between the chemical structure and in vivo characteristics. Biodistribution studies in mice revealed high initial brain uptake for all the compounds. Blood radioactivity level depended markedly upon the chemical stability of the compound. The α, α-dimethylester derivative (1e), amide derivatives (2a-c) and diamine derivatives (3a, b, 4), which were stable to hydrolysis, showed low blood activity levels following i.v. administration. Disappearance of the ester and amide compounds from the brain was rapid. However, the diamine derivatives displayed improved retention in the brain. Compounds 3a and 4 possessed the best combination of high brain uptake and sufficient retention to be useful as potential brain imaging radiopharmaceuticals with SPECT devices.

• 社団法人日本薬学会の論文
• 1989-09-25

著者

• 横山 陽

  Faculty of Pharmaceutical Sciences, Kyoto University

• 間賀田 泰寛

  京都大学医学部

• 大桃 善朗

  Osaka University of Pharmaceutical Sciences

• 田中 千秋

  Osaka University of Pharmaceutical Sciences

• 間賀田 泰寛

  Faculty of Medicine, Kyoto University

• 奥山 慎一郎

  Osaka University of Pharmaceutical Sciences

• 植野 容子

  Osaka University of Pharmaceutical Sciences

• 間賀田 泰寛

  京都大学医学部放射線核医学講座

• 田中 千秋

  Osaka College Of Pharmacy

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